Stable abiraterone oral solid medicinal composition and preparation method thereof

A technology of abiraterone and abiraterone acetate, which is applied in the direction of drug combination, pharmaceutical formula, medical preparations of non-active ingredients, etc.

Inactive Publication Date: 2014-05-21
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007]Although abiraterone acetate is effective in oral treatment of advanced prostate cancer, the poor stability of its preparation during storage has brought serious troubles to the development of preparations
Abiraterone acetate preparations are prone to degraded impurities due to the influence of various complex factors during storage

Method used

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  • Stable abiraterone oral solid medicinal composition and preparation method thereof
  • Stable abiraterone oral solid medicinal composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1~7

[0034] For the prescription of citrate, the detailed prescription is shown in Table 1:

[0035] Table 1 The prescription form of Examples 1-7 (comprising citric acid or its pharmaceutically acceptable salt)

[0036] prescription Example 1 Example 2 Example 3 Example 4 Example 5 Example 6 Example 7 Abiraterone acetate 125mg 250mg 250mg 250mg 250mg 250mg 500mg Sodium citrate (as anhydrous sodium citrate) 1.25mg —— 10mg 12.5mg 16.7mg —— 100mg Potassium citrate (calculated as anhydrous potassium citrate) —— 5mg —— —— —— 25mg —— lactose —— 200mg 200mg 200mg 200mg 200mg —— microcrystalline cellulose —— 160mg 160mg 160mg 160mg 160mg —— Mannitol 250mg —— —— —— —— —— 125mg starch —— —— —— —— —— —— 125mg pregelatinized starch 250mg —— —— —— —— —— —— Croscarmellose Sodium —— 40mg 40mg 40mg 40mg 40mg —— Cros...

Embodiment and

[0067] Embodiment and comparative examples 1-7 place 2 months under the condition of 60 ± 2 ℃ of degraded impurity comparison

[0068] The samples of Examples and Comparative Examples 1-7 placed at 60±2°C for 2 months were measured according to the above-mentioned method for measuring degraded impurities, and the results are shown in Table 3.

[0069] Table 3 Degradation Impurity Determination Results of Examples and Comparative Examples 1-7 placed at 60±2°C for 2 months

[0070]

[0071] Note: * indicates three degradation impurities whose relative retention time with abiraterone acetate is 0.45, 0.57, 0.60.

[0072] The results of the comparison of the degraded impurities in the above examples and comparative examples 1 to 7 show that the three main degraded impurities RRT45, RRT57, and RRT60 was significantly reduced, indicating that citrate can significantly improve the stability of each formulation (composition).

[0073]

Embodiment

[0074] Embodiments and comparative examples 1-7 place 6 months under the condition of 40 ± 2 ℃, RH75% ± 5% degradation impurity comparison

[0075] The samples of Examples and Comparative Examples 1 to 7 placed for 2 months under the conditions of 40±2°C and RH75%±5% were measured according to the above-mentioned determination method of degraded impurities, and the measurement results are shown in Table 4.

[0076] Table 4 Degradation Impurity Determination Results of Examples and Comparative Examples 1-7 placed at 40±2°C for 6 months

[0077]

[0078] Note: * indicates three degradation impurities whose relative retention time with abiraterone acetate is 0.45, 0.57, 0.60.

[0079] The comparative measurement results of the degradation impurities of the above examples and comparative examples 1 to 7 show that at 40 ± 2°C 、 Placed for 6 months under the condition of RH75%±5%, the three main degradation impurities RRT45, RRT57 and RRT60 were significantly reduced after...

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PUM

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Abstract

The invention relates to a stable abiraterone oral solid medicinal composition and a preparation method thereof. The composition comprises abiraterone acetate, citrate and medical auxiliaries. The composition can be used for effectively improving the stability of abiraterone acetate preparations in the storing process, and remarkably reducing generation of degraded impurities.

Description

Technical field [0001] The present invention is a pharmaceutical preparation field, which involves a stable Aibi Dragon oral solid drug composition and its preparation methods. The composition contains acetic acid acteronic acid, citrin, and medicinal auxiliary materials. technical background [0002] Abiratorone acetate, chemical name is: (3β) -17- (3-pyridinyl) -5,16-dilate-3-alcohol acetate. [0003] [0004] [0005] Abbiton can be converted into Aibi Dragon in the body. Aibiram is a cytochrome oxidase P450 (CYP450) C17 inhibitor. By inhibiting the key enzymes in therogen synthesis -CYP450C17, therogen level is reduced, soAbbit dragon not only inhibits the inhibitory effects of the body and other parts of the body, such as adrenal glands. [0006] Asheminals have a promotion effect on the growth of prostate cancer cells. At present, patients with advanced prostate cancer generally preferred to be treated with drugs and surgery to reduce testicular synthetic androgen. Howev...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/58A61K47/12A61K47/38A61P35/00
CPCA61K9/2013A61K31/58A61P35/00
Inventor 王立张涛邓杰
Owner CHONGQING PHARMA RES INST
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